Topical foam composition

Abstract

The present invention relates to a novel oil in water emulsion aerosol foam composition containing an active agent for the treatment of various chronic and acute skin conditions, particularly acne and psoriasis; and processes for preparing the emulsion aerosol foam compositions. In particular, the present invention relates to oil in water emulsion aerosol foam compositions containing a retinoid in the oil phase.

1 . An oil in water emulsion aerosol foam composition comprising an oil phase and a water phase, said composition comprising:
 (i) at least one pharmaceutically active agent which is tazarotene,   (ii) water,   (iii) an oil present in an amount of less than about 10% by weight,   (iv) an oil miscible organic solvent,   (v) a surfactant component comprising a hydrophilic surfactant, in an amount from about 0.1% to about 10% by weight, and   (vi) a propellant; and wherein   the pharmaceutically active agent is solubilized in the oil phase of the composition, and wherein the particle size of the oil phase is less than about 1000 nm.   
     
     
         2 . The aerosol foam composition according to  claim 1 , wherein the composition comprises a second pharmaceutically active agent. 
     
     
         3 . The aerosol foam composition according to  claim 1 , wherein the composition comprises water in an amount from about 65% to about 90% by weight. 
     
     
         4 . The aerosol foam composition according to  claim 3 , wherein the composition comprises water in an amount from about 70% to about 85% by weight. 
     
     
         5 . The aerosol foam composition according to  claim 1 , wherein the oil is selected from the group consisting of azulene, chamazulene, isoparaffin, linear alpha olefins, cyclohexlidenediphenyl methane, didecene, diethylhexylcyclohexane, eicosane, isododecane, isoeicosane, isohexadecane, longifolene, mineral oil, paraffin, pentahydrosqualene, petrolatum, squalane, squalene, tetradecene, and mixtures thereof. 
     
     
         6 . The aerosol foam composition according to  claim 1 , wherein the oil is present in an amount from about 1% to about 9% by weight. 
     
     
         7 . The aerosol foam composition according to  claim 6 , wherein the oil is present in an amount from about 3% to about 8% by weight. 
     
     
         8 . (canceled) 
     
     
         9 . (canceled) 
     
     
         10 . The aerosol foam composition according to  claim 5 , wherein the oil miscible organic solvent is selected from the group consisting of diisopropyl adipate, isopropyl myristate, octyl dodecanol and caprylic/capric triglyceride, and mixtures thereof. 
     
     
         11 . The aerosol foam composition according to  claim 10 , wherein the oil is mineral oil. 
     
     
         12 . The aerosol foam composition according to  claim 1 , wherein the surfactant component is present in amount from about 1% to about 8% by weight. 
     
     
         13 . The aerosol foam composition according to  claim 1 , wherein the surfactant component is present in amount from about 2% to about 6% by weight. 
     
     
         14 . The aerosol foam composition according to  claim 1 , wherein the surfactant component comprises a non-ionic surfactant. 
     
     
         15 . The aerosol foam composition according to  claim 12  wherein the non-ionic surfactant is a PEG derivative, a propylene glycol ester, a fatty alcohol, a glycerol ester or derivative thereof, a polymeric ether, a sorbitan ester or a mixture thereof. 
     
     
         16 . The aerosol foam composition according to  claim 1 , wherein the propellant comprises one or more hydrocarbon propellants. 
     
     
         17 . A method of treating a skin disease, disorder or condition, comprising administering to the skin of a patient requiring such treatment an effective amount of a composition according to  claim 1 . 
     
     
         18 . An oil in water emulsion aerosol foam composition comprising an oil phase and a water phase, said composition comprising:
 i) tazarotene;   ii) water;   iii) an oil selected from the group consisting of azulene, chamazulene, isoparaffin, linear alpha olefins, cyclohexlidenediphenyl methane, didecene, ethylhexylcyclohexane, eicosane, isododecane, isoeicosane, isohexadecane, longifolene, mineral oil, paraffin, pentahydrosqualene, petrolatum, squalane, squalene, tetradecene, and mixtures thereof; and wherein the oil is present in an amount from about 3% to about 8% by weight;   iv) an oil miscible organic solvent selected from the group consisting of diisopropyl adipate, isopropyl myristate, octyl dodecanol and caprylic I capric triglyceride, and mixtures thereof   v) a non-ionic surfactant component comprising a hydrophilic surfactant, in an amount from about 2% to about 6% by weight; and   vi) a hydrocarbon propellant; and   
       wherein the tazarotene is solubilized in the oil phase of the composition, and wherein the particle size of the oil phase is less than about 1000 nm. 
     
     
         19 . A method of treating a skin disease, disorder or condition, comprising administering to the skin of a patient requiring such treatment an effective amount of a composition according to  claim 18 . 
     
     
         20 . A process for the preparation of an oil in water submicron or micro emulsion aerosol foam composition, comprising tazarotene, water, an oil present in an amount of less than about 10% by weight, an oil miscible organic solvent, a surfactant component comprising a hydrophilic surfactant in an amount from about 0.1% to about 10% by weight, and a propellant, the process comprising:
 a. admixing the pharmaceutically active agent, a first aliquot of water, oil, oil miscible organic solvent and surfactant component to form an oil in water emulsion,   b. heating the oil in water emulsion of step (a) to a phase inversion temperature wherein the oil in water emulsion forms a water in oil emulsion,   c. cooling the water in oil emulsion to below the phase inversion temperature to form a submicron or micro oil in water emulsion,   d. adding a second aliquot of water to cool the submicron or micro oil in water emulsion,   e. actuating a sample of the submicron or micro oil in water emulsion with a propellant to form an oil in water submicron or micro emulsion aerosol foam.   
     
     
         21 . The process according to  claim 20 , wherein the first aliquot of water comprises about 10% to about 40% by weight of the total water content of the submicron or micro emulsion aerosol foam and the second aliquot of water comprises about 90% to about 60% by weight of the total water content of the submicron or micro emulsion aerosol foam. 
     
     
         22 . The product produced by the process according to  claim 20 .